Ensaculin

Drugbox
IUPAC_name = 7-methoxy-6- [3- [4-(2-methoxyphenyl)piperazin-1-yl] propoxy] -3,4-dimethylchromen-2-one

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width= 240
CAS_number= 155773-59-4
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PubChem= 208923
DrugBank=
C=26 | H=32 | N=2 | O=5
molecular_weight = 452.543
smiles = CC1=C(C(=O)OC2=CC(=C(C=C12)OCCCN3CCN(CC3)C4=CC=CC=C4OC)OC)C
bioavailability=
metabolism =
elimination_half-life= 13.7 hours
excretion =
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Ensaculin (KA-672) is a drug from the coumarin family, which has been researched as a potential treatment for dementia. It acts on a number of receptor systems, being both a weak NMDA antagonist and a 5HT_1A agonist. [Lishko PV, Maximyuk OP, Chatterjee SS, Nöldner M, Krishtal OA. The putative cognitive enhancer KA-672.HCl is an uncompetitive voltage-dependent NMDA receptor antagonist. "Neuroreport". 1998 Dec 21;9(18):4193-7. PMID 9926872] [Winter JC, Helsley SE, Rabin RA. The discriminative stimulus effects of KA 672, a putative cognitive enhancer: evidence for a 5-HT1A component. "Pharmacology, Biochemistry and Behaviour". 1998 Jul;60(3):703-7. PMID 9678654] Animal studies have shown promising nootropic effects, [Hoerr R, Noeldner M. Ensaculin (KA-672 HCl): a multitransmitter approach to dementia treatment. "CNS Drug Reviews". 2002 Summer;8(2):143-58. PMID 12177685] [Knauber J, Müller WE. Anseculin improves passive avoidance learning of aged mice. "Pharmacological Research". 2003 Mar;47(3):225-33. PMID 12591018] although efficacy in humans has yet to be proven. It was well tolerated in human trials, with the main side effect being othostatic hypotension (low blood pressure). [Sourgens H, Hoerr R, Biber A, Steinbrede H, Derendorf H. KA 672-HCl, a neuronal activator against dementia: tolerability, safety, and preliminary pharmacokinetics after single and multiple oral doses in healthy male and female volunteers. "Journal of Clinical Pharmacology". 1998 Apr;38(4):373-81. PMID 9590466]

References